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TargetRAC-alpha serine/threonine-protein kinase
LigandBDBM11824
Substrate/CompetitorBiotinylated Peptide Substrate
Meas. Tech.PKB In Vitro Kinase Assay
pH7.5±n/a
Temperature295.15±n/a K
IC50 355±n/a nM
Citation Breitenlechner, CBWegge, TBerillon, LGraul, KMarzenell, KFriebe, WGThomas, USchumacher, RHuber, REngh, RAMasjost, B Structure-based optimization of novel azepane derivatives as PKB inhibitors. J Med Chem47:1375-90 (2004) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
RAC-alpha serine/threonine-protein kinase
Name:RAC-alpha serine/threonine-protein kinase
Synonyms:AKT phosphorylation (p-AKT) | C-AKT | PKB | PKB alpha | Protein kinase Akt-1 | Protein kinase B | Protein kinase B (AKT1) | Protein kinase B (Akt 1) | Protein kinase B (Akt) | Protein kinase B alpha | Protein kinase B alpha (AKT1) | Proto-oncogene Akt (Akt1) | Proto-oncogene c-Akt (AKT) | Proto-oncogene c-Akt (AKT1) | RAC-PK-alpha | RAC-alpha serine/threonine-protein kinase (AKT) | RAC-alpha serine/threonine-protein kinase (AKT1) | RAC-alpha serine/threonine-protein kinase (pAKT)
Type:Enzyme
Mol. Mass.:55681.25
Organism:Homo sapiens (Human)
Description:P31749
Residue:480
Sequence:
MSDVAIVKEGWLHKRGEYIKTWRPRYFLLKNDGTFIGYKERPQDVDQREAPLNNFSVAQC
QLMKTERPRPNTFIIRCLQWTTVIERTFHVETPEEREEWTTAIQTVADGLKKQEEEEMDF
RSGSPSDNSGAEEMEVSLAKPKHRVTMNEFEYLKLLGKGTFGKVILVKEKATGRYYAMKI
LKKEVIVAKDEVAHTLTENRVLQNSRHPFLTALKYSFQTHDRLCFVMEYANGGELFFHLS
RERVFSEDRARFYGAEIVSALDYLHSEKNVVYRDLKLENLMLDKDGHIKITDFGLCKEGI
KDGATMKTFCGTPEYLAPEVLEDNDYGRAVDWWGLGVVMYEMMCGRLPFYNQDHEKLFEL
ILMEEIRFPRTLGPEAKSLLSGLLKKDPKQRLGGGSEDAKEIMQHRFFAGIVWQHVYEKK
LSPPFKPQVTSETDTRYFDEEFTAQMITITPPDQDDSMECVDSERRPHFPQFSYSASGTA
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM11824
NameBDBM11824
Synonyms:Azepane Derivative 5 | N-((3R,4R)-4-{[4-(2-fluoro-6-hydroxy-3-methoxybenzoyl)benzyl]oxy}azepan-3-yl)isonicotinamide dihydrochloride | N-[(3R,4R)-4-({4-[(2-fluoro-6-hydroxy-3-methoxyphenyl)carbonyl]phenyl}methoxy)azepan-3-yl]pyridine-4-carboxamide dihydrochloride
TypeSmall organic molecule
Emp. Form.C27H28FN3O5
Mol. Mass.493.5267
SMILESCOc1ccc(O)c(C(=O)c2ccc(CO[C@@H]3CCCNC[C@H]3NC(=O)c3ccncc3)cc2)c1F |r|
Structure
Biotinylated Peptide Substrate
Name:Biotinylated Peptide Substrate
Synonyms:n/a
Type:Peptide
Mol. Mass.:1764.91
Organism:n/a
Description:n/a
Residue:17
Sequence:
Biotin-SGRARTSSFAEPG